Oclacitinib maleate (PF-03394197 maleate, PF03394197 maleate),又称奥拉替尼马来酸盐,是一种新型可口服的JAK抑制剂,IC50分别为10-99 nM,对JAK1最有效,IC50为10 nM。Oclacitinib也能抑制JAK1依赖性细胞因子,IC50为36-249 nM。Oclacitinib maleate可用于各种瘙痒性皮肤病,快速止痒抗炎。
参考文献
1.Gonzales AJ, et al. Oclacitinib (APOQUEL) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J Vet Pharmacol Ther. 2014 Aug;37(4):317-24.
2.Fukuyama T, et al. Topically Administered Janus-Kinase Inhibitors Tofacitinib and Oclacitinib Display Impressive Antipruritic and Anti-Inflammatory Responses in a Model of Allergic Dermatitis. J Pharmacol Exp Ther. 2015 Sep;354(3):394-405.
3.Cosgrove SB, et al. Efficacy and safety of oclacitinib for the control of pruritus and associated skin lesions in dogs with canine allergic dermatitis. Vet Dermatol. 2013 Oct;24(5):479-e114.
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。